AR090240A1 - Derivados de triazolopirazina - Google Patents

Derivados de triazolopirazina

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Publication number
AR090240A1
AR090240A1 ARP130100705A ARP130100705A AR090240A1 AR 090240 A1 AR090240 A1 AR 090240A1 AR P130100705 A ARP130100705 A AR P130100705A AR P130100705 A ARP130100705 A AR P130100705A AR 090240 A1 AR090240 A1 AR 090240A1
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AR
Argentina
Prior art keywords
denotes
phet1
hal
atoms
het
Prior art date
Application number
ARP130100705A
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English (en)
Inventor
Dr Schieman Kai
Dr Deutsch Carl
Dr Hoelzemann Guenter
Dr Kuhn Daniel
Dr Wegener Ansgar
Swinnen Dominique
Comas Horacio
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Merck Patent Ges Mit Beschränkter Haftung
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Application filed by Merck Patent Ges Mit Beschränkter Haftung filed Critical Merck Patent Ges Mit Beschränkter Haftung
Publication of AR090240A1 publication Critical patent/AR090240A1/es

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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Abstract

Los compuestos de la fórmula (1) en donde R¹ denota Ar, COHet o Het; R² denota H, Ar¹, NHHet o Het; R³ denota H o A; R⁴ denota H, A, Ar¹, Het, Hal, NHAr¹ o CN; Ar denota fenilo o naftilo que no está sustituido o que está mono- o disustituido con Hal, A, Cyc. [C(R³)₂]ₚOA, [C(R³)₂]ₚOH, CN. NHCOHet¹, NHCOA, NHCO[C(R³)₂]ₚCyc, CONH[C(R³)₂]ₚCyc, [C(R³)₂]ₚN(R³)₂, [C(R³)₂]ₚHet¹, NR³SO₂A, SO₂N(R³)₂, S(O)ₙA, COHet¹, O[C(R³)₂]ₘN(R³)₂ y/u O[C(R³)₂]ₚHet¹; Ar¹ denota fenilo que no está sustituido o que está mono- o disustituido con Hal, A, fenilo, CONH₂ [C(R³)₂]ₚOR³, [C(R³)₂]ₚN(R³)₂, [C(R³)₂]ₚCN, [C(R³)₂]ₚHet¹ y/u O[C(R³)₂]ₚHet¹; Het denota furilo, tienilo, pirrolilo, imidazolilo, pirazolilo, oxazolilo, isoxazolilo, oxadiazolilo, tiazolilo, triazolilo, tetrazolilo, piridilo, pirimidilo, piridazinilo, pirazinilo. indolilo, isoindolilo, bencimidazolilo, indazolilo, quinolilo, 1,3-benzo-dioxolilo, benzotiofenilo, benzofuranilo, imidazopiridilo, dihidroindolilo, 2,3-dihidro-benzo[1,4]dioxinilo o furo[3,2-b]piridilo que no está sustituido o que está mono-, di- o trisustituido con Hal, A, [C(R³)₂]ₚOR³, [C(R³)₂]ₚN(R³)₂, [C(R³)₂]ₚHet¹, NO₂, CN, [C(R⁶)₂]ₚCOOR³, CON(R³)₂, NR³COA, NR³SO₂A, SO₂N(R³)₂, S(O)ₙA, COHet¹, O[C(R³)₂]ₘN(R³)₂, O[C(R³)₂]ₚHet¹ y/u =O; Het¹ denota dihidropirrolilo, pirrolidinilo, azetidinilo, oxetanilo, tetrahidroimidazolilo, dihidropirazolilo, tetrahidropirazolilo, tetrahidrofuranilo, dihidropiridilo, tetrahidropiridilo, piperidinilo, morfolinilo, hexahidropiridazinilo. hexahidropirimidinilo, [1,3]dioxolanilo, tetrahidropiranilo, piridilo o piperazinilo que no está sustituido o que está mono- o disustituido con Hal, CN, OH, OA, COOA, CONH₂, S(O)ₙA, S(O)ₙAr, COA, A y/u =O; A denota alquilo no ramificado o ramificado con 1-10 átomos de C, en donde uno o dos grupos no adyacentes CH y/o CH₂ pueden estar reemplazados por átomos de N, O y/o S y en donde 1 - 7 átomos de H pueden estar reemplazados por F o Cl; Cyc denota alquilo cíclico con 3-7 átomos de C, que no está sustituido o que está monosustituido con [C(R³)₂]ₚOH o CN; A denota alquilo no ramificado o ramificado con 1, 2, 3 ó 4 átomos de C; Hal denota F, Cl, Br o I; n denota 0, 1 ó 2; m denota 1, 2 ó 3; p denota 0, 1, 2, 3 ó 4; y sus solvatos, sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de GCN2 y se pueden emplear, inter alia, para el tratamiento de cáncer.
ARP130100705A 2012-03-07 2013-03-05 Derivados de triazolopirazina AR090240A1 (es)

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EP12001568 2012-03-07

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AR090240A1 true AR090240A1 (es) 2014-10-29

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US (1) US20150051202A1 (es)
EP (1) EP2822948B1 (es)
JP (1) JP6049768B2 (es)
CN (1) CN104159901B (es)
AR (1) AR090240A1 (es)
AU (1) AU2013230286B2 (es)
CA (1) CA2866450C (es)
ES (1) ES2579981T3 (es)
HK (1) HK1203948A1 (es)
IL (1) IL234466A (es)
TW (1) TW201341384A (es)
WO (1) WO2013131609A1 (es)

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